Synthesis of N-(2-diethylamino-ethyl)-4-(4-fluoro-benzamido)-2-methoxybenzamide (desiodo-MIP-1145) by coupling technique and its radioiodination: a potential melanoma imaging agent.

Radioiodinated MIP-1145, which specifically targets melanin, is an ideal candidate for targeted therapy of melanoma. An analogue of MIP-1145 lacking the iodo-substituent (desiodo-MIP-1145) was synthesized as a labeling precursor in three simple steps. The radioiodination of desiodo-MIP-1145 by iodine-125 was carried out via an electrophilic substitution reaction.

Optimization of solid-phase synthesis of difficult peptide sequences via comparison between different improved approaches.

Different approaches are applied to avoid the strong aggregation of the difficult peptide sequences, which is considered as the main reason for incomplete acylation and deprotection reactions hindering the synthesis of these sequences. Temporary protection of amide nitrogen of peptide bond using 2-hydroxy-4-methoxybenzyl (Hmb) and 2,4,6-timethoxybenzyl (Tmob) amino acid derivatives, introduction of D-Ala or Pro residues in the peptide chain sequences and utilization of microwave energy are proved to be useful methods in the enhancement of solubility and in the hindrance of the aggregation during the solid-phase synthesis of oligoalanine. Oligoalanine is chosen to demonstrate the difficult sequences and to compare the efficiencies of these methods.

Optimized conventional synthesis of "RGD" and "RGDS" peptides and their sarcosine mimics as integrin GP IIb/IIIa antagonists.

Synthetic arginyl-glycyl- alpha-aspartyl "RGD" and arginyl-glycyl- alpha-aspartyl-serinyl "RGDS" peptide sequences, which are originally located in matrix proteins, are confirmed to be as versatile integrin GP IIb/IIIa antagonists. Since integrins, as cell surface glycoprotein receptors are implicated in several physiological mechanisms, these peptides are recently specially considered in the design of new therapeutics. Replacing glycine by sarcosine, as its more lipophilic isomer, in RGD peptides seemed, accordingly, interesting in revealing some structural/biological activity relationships.

Tricho-dento-osseous syndrome: a scanning electron microscopic analysis.

A large kindred of which multiple members have the Tricho-dento-osseous syndrome is presented. This is an autosomal dominant disorder characterized by defective enamel, taurodontia, unusually curly hair and occasionally mild to moderate skeletal osteosclerosis. Histologic investigation of teeth (by both LM and SEM) demonstrated that there is a uniformly thin enamel covering with randomly distributed depression and pits.